Abarelix is a synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It directly and competitively binds and blocks the gonadotropin releasing hormone receptors in the anterior pituitary, which inhibits the secretion and release of the luteinizing hormone (LH) and follicle stimulating hormone (FSH). For men, the inhibition of LH secretion prevents the release of testosterone. Therefore, it can relieve symptoms associated with prostate hypertrophy or prostate cancer.
CAT No: 10-101-60
CAS No:183552-38-7
Synonyms/Alias:Abarelix;183552-38-7;Plenaxis;PPI-149;Plenaxis depot;PPI 149;R 3827;R-3827;UNII-W486SJ5824;CHEBI:337298;R3827;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-;CHEMBL1252;PPI149;DTXSID20171443;W486SJ5824;N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N(sup 6)-isopropyl-L-lysyl-L-prolyl-D-alaninamide;R382;R-382;N-acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparginyl-L-leucyl-N(6)-isopropyl-L-lysyl-L-prolyl-D-alaninamide;Abarelix-Depot-M;Abarelix Trifluoroacetate Salt (~90%);Plenaxis (TN);Abarelix (USAN/INN);Abarelix [USAN:INN];abarelixum;N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparginyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide;SCHEMBL9533;GTPL1188;DTXCID4093934;SCHEMBL19712245;L02XB01;AIWRTTMUVOZGPW-HSPKUQOVSA-N;Abarelix acetate - Bio-X trade mark;BDBM50102442;AKOS040732360;R3827;PPI 149;AT36700;CS-5873;DB00106;FA55835;BA300028;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl- 10;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-10;HY-13534;MS-32159;D02738;EN300-20605823;Q305555;Ac-D-Nal-[D-(pCl)Phe]-D-Pal-Ser-[Nalpha-Me-Tyr]-D-Asn-Leu-ILys-Pro-DAla-NH2;N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N(6)-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide;
Chemical Name:(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide
Abarelix, also known as a gonadotropin-releasing hormone (GnRH) antagonist, is a synthetic decapeptide widely recognized for its ability to modulate hormone signaling pathways. As a potent blocker of GnRH receptors, Abarelix effectively inhibits the downstream release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary gland. This targeted mode of action makes it a valuable research reagent in studies exploring the regulation of reproductive hormones and endocrine feedback mechanisms. Its chemical stability, high specificity, and rapid onset of action have positioned Abarelix as a preferred tool for in vitro and in vivo experimental models investigating hormonal control systems.
Endocrine Research: In endocrine system research, Abarelix serves as an essential probe for dissecting the physiological roles of GnRH and its downstream effectors. By selectively antagonizing the GnRH receptor, it enables researchers to observe the immediate and long-term effects of gonadotropin suppression on pituitary and gonadal function. This approach provides insights into the regulatory circuits governing hormone secretion, feedback inhibition, and receptor desensitization, facilitating the development of novel hypotheses regarding endocrine homeostasis.
Oncology Studies: Within oncology research, Abarelix is frequently employed to model androgen deprivation conditions, particularly in hormone-dependent cancer cell lines. Its ability to rapidly lower LH and FSH secretion creates an experimental environment that mimics androgen ablation, allowing scientists to evaluate tumor cell responses, gene expression changes, and resistance mechanisms under reduced hormonal stimulation. This application aids in the identification of new molecular targets and therapeutic strategies for hormone-sensitive malignancies.
Reproductive Biology: In the field of reproductive biology, GnRH antagonists like Abarelix are utilized to manipulate the hypothalamic-pituitary-gonadal axis in animal models. Through precise temporal control of gonadotropin release, researchers can investigate processes such as folliculogenesis, spermatogenesis, and gamete maturation. These studies contribute to a more comprehensive understanding of reproductive physiology, fertility regulation, and the effects of exogenous hormone modulation on reproductive outcomes.
Pharmacological Profiling: Abarelix is also an important tool in pharmacological profiling and drug discovery. By serving as a reference antagonist, it facilitates the screening and characterization of novel GnRH analogs, receptor modulators, and downstream signaling inhibitors. Comparative studies using this decapeptide help elucidate structure-activity relationships, receptor binding affinities, and the pharmacodynamic properties of candidate compounds, accelerating the development of next-generation therapeutics targeting the GnRH pathway.
Signal Transduction Studies: In cellular signaling research, Abarelix is instrumental in delineating the molecular cascades initiated by GnRH receptor engagement. Its application in signal transduction assays allows researchers to map the downstream pathways activated or suppressed in the presence of a GnRH antagonist. This information is critical for understanding the cross-talk between hormonal signals and other cellular processes, including proliferation, differentiation, and apoptosis, thereby expanding the knowledge base required for targeted intervention in hormone-responsive tissues. Through these diverse applications, Abarelix continues to be an indispensable asset in advancing the frontiers of endocrine, oncological, reproductive, and pharmacological research.
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